Gregory K Bosch

Publications (2)5.11 Total impact

• Article: Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors.

  Steven V O'Neil, Yili Wang, Michael C Laufersweiler, Kofi A Oppong, David L Soper, John A Wos, Christopher D Ellis, Mark W Baize, Gregory K Bosch, Amy N Fancher, Wei Lu, Maureen K Suchanek, Richard L Wang, Biswanath De, Thomas P Demuth
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  ABSTRACT: Two novel 8,6-fused bicyclic peptidomimetic ring systems were synthesized utilizing olefin metathesis as the key reaction for the formation of the eight-membered ring. Both peptidomimetic scaffolds were further elaborated into potent ICE inhibitors, with numerous compounds exhibiting caspase-1 IC(50)s less than 10nM.
  Bioorganic & Medicinal Chemistry Letters 01/2006; 15(24):5434-8. · 2.55 Impact Factor
• Article: Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis.

  Kofi A Oppong, Christopher D Ellis, Michael C Laufersweiler, Steven V O'Neil, Yili Wang, David L Soper, Mark W Baize, John A Wos, Biswanath De, Gregory K Bosch, Amy N Fancher, Wei Lu, Maureen K Suchanek, Richard L Wang, Thomas P Demuth
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  ABSTRACT: A novel diazocan containing dipeptide mimetic was synthesized via reductive N-N bond cleavage of a pyrazolidino-pyrazolidine using Raney-Ni and evaluated as an ICE inhibitor. This versatile 8-membered ring containing scaffold possesses an N-5 ring nitrogen that was used to explore structure-activity relationships in a cell-based assay measuring inhibition of interleukin-1beta.
  Bioorganic & Medicinal Chemistry Letters 11/2005; 15(19):4291-4. · 2.55 Impact Factor